4.5 Article

Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 2, 页码 333-336

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.11.005

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20-HETE

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In a previous paper, we reported that an imidazole derivative I exhibited a potent inhibitory activity of 20-HETE synthase (1; IC50 value of 5.7 nM), but this compound also exhibited little selectivity for cytochrome P450s (CYPs). We examined some derivatives of imidazole I which had an amino group on the side chain, and found that a dimethylaminohexyloxy derivative (3g ;IC50 value of 8.8 nM) showed potent and selective inhibitory activity. (C) 2003 Elsevier Ltd. All rights reserved.

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